US2024197667A1PendingUtilityA1

Systems and methods for treating vitiligo using ethyl pyruvate and other compounds

Assignee: TRANSDERMAL BIOTECHNOLOGY INCPriority: Apr 14, 2021Filed: Apr 13, 2022Published: Jun 20, 2024
Est. expiryApr 14, 2041(~14.7 yrs left)· nominal 20-yr term from priority
A61K 47/24A61K 9/107A61K 9/0014A61K 31/22A61K 9/127A61K 9/06
61
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Claims

Abstract

The present disclosure generally relates to systems and methods for treating vitiligo. In one set of embodiments, the present disclosure comprises a composition comprising ethyl pyruvate. The composition may be formulated for application to the skin of a subject, for instance, as a gel, lotion, cream, ointment, soap, or stick. In some cases, the composition may comprise a lecithin, such as phosphatidylcholine. In certain embodiments. the lecithin is present as a liquid crystal, and/or in liposomes, micelles, or other vesicles. Other aspects of the present disclosure are generally directed to methods of making or using such compositions, methods of promoting such compositions, kits including such compositions, or the like.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
         1 . A method, comprising:
 applying, to the skin of a subject having vitiligo, a topical composition comprising ethyl pyruvate.   
     
     
         2 . The method of  claim 1 , wherein the ethyl pyruvate is present at less than about 0.2% by weight. 
     
     
         3 . The method of any one of  claim 1 or 2 , wherein the composition comprises a gel, lotion, cream, ointment, soap, or stick. 
     
     
         4 . The method of any one of  claims 1-3 , wherein the formulation is substantially transparent. 
     
     
         5 . The method of any one of  claims 1-4 , wherein the composition comprises a first phase and a second phase. 
     
     
         6 . The method of  claim 5 , wherein the formulation comprises an emulsion of the first phase and a second phase. 
     
     
         7 . The method of any one of  claims 1-6 , wherein the first phase forms discrete vesicles contained within the second phase. 
     
     
         8 . The method of any one of  claims 1-7 , wherein the first phase forms liposomes within the second phase. 
     
     
         9 . The method of any one of  claims 1-8 , wherein the first phase forms multilamellar liposomes within the second phase. 
     
     
         10 . The method of any one of  claims 1-9 , wherein the formulation comprises a liquid crystal structure of the first phase and a second phase. 
     
     
         11 . The method of  claim 10 , wherein at least a portion of the liquid crystal structure is multilamellar. 
     
     
         12 . The method of any one of  claims 1-11 , wherein the composition further comprises lecithin. 
     
     
         13 . The method of  claim 12 , wherein the lecithin is present at at least about 0.25% by weight of the formulation. 
     
     
         14 . The method of any one of  claims 1-13 , wherein the lecithin is present at at least about 1% by weight of the formulation. 
     
     
         15 . The method of any one of  claims 1-14 , wherein the lecithin is present at at least about 10% by weight of the formulation. 
     
     
         16 . The method of any one of  claims 1-15 , wherein the lecithin is present at at least about 30% by weight of the formulation. 
     
     
         17 . The method of any one of  claims 1-16 , wherein the lecithin is present at at least about 60% by weight of the formulation. 
     
     
         18 . The method of any one of  claims 1-17 , wherein the lecithin comprises phosphatidylcholine. 
     
     
         19 . The method of  claim 18 , wherein at least some of the phosphatidylcholine comprises a phosphatidylcholine comprising a stearic diglyceride linked to a choline ester of a phosphoric acid. 
     
     
         20 . The method of any one of  claim 18 or 19 , wherein at least some of the phosphatidylcholine comprises a phosphatidylcholine comprising a palmitic diglyceride linked to a choline ester of a phosphoric acid. 
     
     
         21 . The method of any one of  claims 18-20 , wherein at least some of the phosphatidylcholine comprises a phosphatidylcholine comprising an oleic diglyceride linked to a choline ester of a phosphoric acid. 
     
     
         22 . The method of any one of  claims 1-21 , wherein the lecithin comprises polyenylphosphatidylcholine. 
     
     
         23 . The method of  claim 22 , wherein the polyenylphosphatidylcholine is present at between 0% and about 15% by weight of the formulation. 
     
     
         24 . The method of any one of  claim 22 or 23 , wherein the polyenylphosphatidylcholine comprises linoleic acid. 
     
     
         25 . The method of any one of  claims 22-24 , wherein the polyenylphosphatidylcholine comprises dilinoleoylphosphatidylcholine. 
     
     
         26 . The method of any one of  claims 1-25 , wherein the formulation further comprises an emulsifier. 
     
     
         27 . The method of any one of  claims 1-26 , wherein the formulation further comprises a fatty acid ester. 
     
     
         28 . The method of any one of  claims 1-27 , wherein the formulation further comprises ascorbate palmitate. 
     
     
         29 . The method of any one of  claims 1-28 , wherein the formulation further comprises isopropyl palmitate. 
     
     
         30 . The method of any one of  claims 1-29 , wherein the formulation further comprises a transdermal penetration enhancer. 
     
     
         31 . The method of any one of  claims 1-30 , wherein the formulation further comprises 1,3-dimethyl-2-imidazolidinone. 
     
     
         32 . The method of any one of  claims 1-31 , wherein the formulation further comprises 1,2-propanediol. 
     
     
         33 . The method of any one of  claims 1-32 , wherein the composition has a viscosity of at least about 20,000 cP. 
     
     
         34 . The method of any one of  claims 1-33 , wherein the subject is human. 
     
     
         35 . A composition for transdermal delivery, the composition comprising:
 a transdermal formulation comprising a first phase and a second phase, the first phase comprising water and ethyl pyruvate, the second phase being substantially immiscible with the first phase, the formulation further comprising a surfactant comprising lecithin.   
     
     
         36 . The composition of  claim 35 , wherein the ethyl pyruvate is present at less than about 0.2% by weight. 
     
     
         37 . The composition of any one of  claim 35 or 36 , wherein the composition comprises a gel, lotion, cream, ointment, soap, or stick. 
     
     
         38 . The composition of any one of  claims 35-37 , wherein the formulation is substantially transparent. 
     
     
         39 . The composition of any one of  claims 35-38 , wherein the composition comprises a first phase and a second phase. 
     
     
         40 . The composition of any one of  claims 39 , wherein the formulation comprises an emulsion of the first phase and a second phase. 
     
     
         41 . The composition of any one of  claim 39 or 40 , wherein the first phase forms discrete vesicles contained within the second phase. 
     
     
         42 . The composition of any one of  claims 39-41 , wherein the first phase forms liposomes within the second phase. 
     
     
         43 . The composition of any one of  claims 39-42 , wherein the first phase forms multilamellar liposomes within the second phase. 
     
     
         44 . The composition of any one of  claims 39-43 , wherein the formulation comprises a liquid crystal structure of the first phase and a second phase. 
     
     
         45 . The composition of  claim 44 , wherein at least a portion of the liquid crystal structure is multilamellar. 
     
     
         46 . The composition of  claim 45 , wherein the composition further comprises lecithin. 
     
     
         47 . The composition of  claim 46 , wherein the lecithin is present at at least about 0.25% by weight of the formulation. 
     
     
         48 . The composition of any one of  claims 35-47 , wherein the lecithin is present at at least about 1% by weight of the formulation. 
     
     
         49 . The composition of any one of  claims 35-48 , wherein the lecithin is present at at least about 10% by weight of the formulation. 
     
     
         50 . The composition of any one of  claims 35-49 , wherein the lecithin is present at at least about 30% by weight of the formulation. 
     
     
         51 . The composition of any one of  claims 35-50 , wherein the lecithin is present at at least about 60% by weight of the formulation. 
     
     
         52 . The composition of any one of  claims 35-51 , wherein the lecithin comprises phosphatidylcholine. 
     
     
         53 . The composition of  claim 52 , wherein at least some of the phosphatidylcholine comprises a phosphatidylcholine comprising a stearic diglyceride linked to a choline ester of a phosphoric acid. 
     
     
         54 . The composition of  claim 52 , wherein at least some of the phosphatidylcholine comprises a phosphatidylcholine comprising a palmitic diglyceride linked to a choline ester of a phosphoric acid. 
     
     
         55 . The composition of any one of  claims 52-53 , wherein at least some of the phosphatidylcholine comprises a phosphatidylcholine comprising an oleic diglyceride linked to a choline ester of a phosphoric acid. 
     
     
         56 . The composition of any one of  claims 35-54 , wherein the lecithin comprises polyenylphosphatidylcholine. 
     
     
         57 . The composition of  claim 56 , wherein the polyenylphosphatidylcholine is present at between 0% and about 15% by weight of the formulation. 
     
     
         58 . The composition of  claim 57 , wherein the polyenylphosphatidylcholine comprises linoleic acid. 
     
     
         59 . The composition of any one of  claim 57 or 58 , wherein the polyenylphosphatidylcholine comprises dilinoleoylphosphatidylcholine. 
     
     
         60 . The composition of any one of  claims 35-59 , wherein the formulation further comprises an emulsifier. 
     
     
         61 . The composition of any one of  claims 35-60 , wherein the formulation further comprises a fatty acid ester. 
     
     
         62 . The composition of any one of  claims 35-61 , wherein the formulation further comprises ascorbate palmitate. 
     
     
         63 . The composition of any one of  claims 35-62 , wherein the formulation further comprises isopropyl palmitate. 
     
     
         64 . The composition of any one of  claims 35-63 , wherein the formulation further comprises a transdermal penetration enhancer. 
     
     
         65 . The composition of any one of  claims 35-64 , wherein the formulation further comprises 1,3-dimethyl-2-imidazolidinone. 
     
     
         66 . The composition of any one of  claims 35-65 , wherein the formulation further comprises 1,2-propanediol. 
     
     
         67 . The composition of any one of  claims 35-66 , wherein the composition has a viscosity of at least about 20,000 cP. 
     
     
         68 . A composition for transdermal delivery, the composition comprising:
 a cream comprising a first phase and a second phase, the first phase comprising water and ethyl pyruvate, the second phase being substantially immiscible with the first phase, the cream further comprising polyenylphosphatidylcholine stabilizing the first phase and the second phase.   
     
     
         69 . The composition of  claim 68 , wherein the ethyl pyruvate is present at less than about 0.2% by weight. 
     
     
         70 . The composition of any one of  claim 68 or 69 , wherein the composition comprises a gel, lotion, cream, ointment, soap, or stick. 
     
     
         71 . The composition of any one of  claims 68-70 , wherein the formulation is substantially transparent. 
     
     
         72 . The composition of any one of  claims 68-71 , wherein the composition comprises a first phase and a second phase. 
     
     
         73 . The composition of  claim 72 , wherein the formulation comprises an emulsion of the first phase and a second phase. 
     
     
         74 . The composition of any one of  claims 68-73 , wherein the first phase forms discrete vesicles contained within the second phase. 
     
     
         75 . The composition of any one of  claims 68-74 , wherein the first phase forms liposomes within the second phase. 
     
     
         76 . The composition of any one of  claims 68-75 , wherein the first phase forms multilamellar liposomes within the second phase. 
     
     
         77 . The composition of  claim 76 , wherein the formulation comprises a liquid crystal structure of the first phase and a second phase. 
     
     
         78 . The composition of  claim 77 , wherein at least a portion of the liquid crystal structure is multilamellar. 
     
     
         79 . The composition of any one of  claims 68-78 , wherein the composition further comprises lecithin. 
     
     
         80 . The composition of  claim 79 , wherein the lecithin is present at at least about 0.25% by weight of the formulation. 
     
     
         81 . The composition of any one of  claims 68-80 , wherein the lecithin is present at at least about 1% by weight of the formulation. 
     
     
         82 . The composition of any one of  claims 68-81 , wherein the lecithin is present at at least about 10% by weight of the formulation. 
     
     
         83 . The composition of any one of  claims 68-82 , wherein the lecithin is present at at least about 30% by weight of the formulation. 
     
     
         84 . The composition of any one of  claims 68-83 , wherein the lecithin is present at at least about 60% by weight of the formulation. 
     
     
         85 . The composition of any one of  claims 68-84 , wherein the lecithin comprises phosphatidylcholine. 
     
     
         86 . The composition of  claim 85 , wherein at least some of the phosphatidylcholine comprises a phosphatidylcholine comprising a stearic diglyceride linked to a choline ester of a phosphoric acid. 
     
     
         87 . The composition of any one of  claim 85 or 86 , wherein at least some of the phosphatidylcholine comprises a phosphatidylcholine comprising a palmitic diglyceride linked to a choline ester of a phosphoric acid. 
     
     
         88 . The composition of any one of  claim 85-87 , wherein at least some of the phosphatidylcholine comprises a phosphatidylcholine comprising an oleic diglyceride linked to a choline ester of a phosphoric acid. 
     
     
         89 . The composition of any one of  claims 68-88 , wherein the lecithin comprises polyenylphosphatidylcholine. 
     
     
         90 . The composition of  claim 89 , wherein the polyenylphosphatidylcholine is present at between 0% and about 15% by weight of the formulation. 
     
     
         91 . The composition of any one of  claim 89 or 90 , wherein the polyenylphosphatidylcholine comprises linoleic acid. 
     
     
         92 . The composition of any one of  claims 89-91 , wherein the polyenylphosphatidylcholine comprises dilinoleoylphosphatidylcholine. 
     
     
         93 . The composition of any one of  claims 68-92 , wherein the formulation further comprises an emulsifier. 
     
     
         94 . The composition of any one of  claims 68-93 , wherein the formulation further comprises a fatty acid ester. 
     
     
         95 . The composition of any one of  claims 68-94 , wherein the formulation further comprises ascorbate palmitate. 
     
     
         96 . The composition of any one of  claims 68-95 , wherein the formulation further comprises isopropyl palmitate. 
     
     
         97 . The composition of any one of  claims 68-96 , wherein the formulation further comprises a transdermal penetration enhancer. 
     
     
         98 . The composition of any one of  claims 68-97 , wherein the formulation further comprises 1,3-dimethyl-2-imidazolidinone. 
     
     
         99 . The composition of any one of  claims 68-98 , wherein the formulation further comprises 1,2-propanediol. 
     
     
         100 . The composition of any one of  claims 68-99 , wherein the composition has a viscosity of at least about 20,000 cP.

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